IGNITING INNOVATION

for a remarkable difference in scientific discovery

IGNITING INNOVATION

for a remarkable difference in scientific discovery

EXPANDING THE FRONTIERS OF KNOWLEDGE

There is no guarantee in drug discovery but we seek to improve the odds so we have a greater chance of success.

Allen Reitz, Ph.D., CEO

DOCUMENTS

PUBLICATIONS

Guan H, Nuth M, Scott RW, Parker MH, Strobel ED, Reitz AB, Kulp JL 3rd, Ricciardi RP. Potency of a small molecule that targets the molluscum contagiosum virus processivity factor increases when conjugated to a tripeptide. Antiviral Res. 2024 Jun;226:105899. doi: 10.1016/j.antiviral.2024.105899.

Eddy K, Gupta K, Eddin MN, Marinaro C, Putta S, Sauer JM Jr, Chaly A, Freeman KB, Pelletier JC, Fateeva A, Furmanski P, Silk AW, Reitz AB, Zloza A, Chen S. Assessing Longitudinal Treatment Efficacies and Alterations in Molecular Markers Associated with Glutamatergic Signaling and Immune Checkpoint Inhibitors in a Spontaneous Melanoma Mouse Model. JID Innov. 2024 Jan 18;4(2):100262. doi: 10.1016/j.xjidi.2024.100262.

Shields BC, Yan H, Lim SSX, Burwell SCV, Cammarata CM, Fleming EA, Yousefzadeh SA, Goldenshtein VZ, Kahuno EW, Vagadia PP, Loughran MH, Zhiquan L, McDonnell ME, Scalabrino ML, Thapa M, Hawley TM, Field GD, Hull C, Schiltz GE, Glickfeld LL, Reitz AB, Tadross MR. DART.2: bidirectional synaptic pharmacology with thousandfold cellular specificity. Nat Methods. 2024 Jul;21(7):1288-1297. doi: 10.1038/s41592-024-02292-9.

Emert-Sediak, L. A.; Tice, C. M.; Shi, H.; Alvarado, J. J.; Shu, S. T.; Reitz, A. B.; Smithgall, T. E. PROTAC-mediated degradation of HIV-1 Nef efficiently restores cell-surface CD4 and MHC-I expression and blocks HIV-1 replication. Cell Chem. Biol. 2024, 31, 1-11. doi:10.1016/j.chembiol.2024.02.004.

Eddy, K.; Gupta, K.; Pelletier, J. C.; Isola, A. L.; Marinaro, C.; Rasheed, M. A.; Campagnolo, J.; Eddin, M. N.; Rossi, N.; Fateeva, A.; Reuhl,, K.; Shah, R.; Robinson, A. K.; Chaly, A.; Freeman, K. B.; Chen, W.; Diaz, J.; Furmanski, P.; Silk, A. W.; Reitz, A. B.; Zloza, A.; Chen. S. A Spontaneous Melanoma Mouse Model Applicable for a longitudinal Chemotherapy and Immunotherapy Study. J. Investigative Dermatology, 2023, 143, 2007-2018. DOI: 10.1016/j.jid.2023.03.1664.

LIST OF SELECTED PUBLICATIONS

SELECTED PUBLICATIONS

Emert-Sediak, L. A.; Tice, C. M.; Shi, H.; Alvarado, J. J.; Shu, S. T.; Reitz, A. B.; Smithgall, T. E. PROTAC-mediated degradation of HIV-1 Nef efficiently restores cell-surface CD4 and MHC-I expression and blocks HIV-1 replication. Cell Chem. Biol. 2024, 31, 1-11. doi:10.1016/j.chembiol.2024.02.004.

Eddy, K.; Gupta, K.; Pelletier, J. C.; Isola, A. L.; Marinaro, C.; Rasheed, M. A.; Campagnolo, J.; Eddin, M. N.; Rossi, N.; Fateeva, A.; Reuhl,, K.; Shah, R.; Robinson, A. K.; Chaly, A.; Freeman, K. B.; Chen, W.; Diaz, J.; Furmanski, P.; Silk, A. W.; Reitz, A. B.; Zloza, A.; Chen. S. A Spontaneous Melanoma Mouse Model Applicable for a longitudinal Chemotherapy and Immunotherapy Study. J. Investigative Dermatology, 2023, 143, 2007-2018. DOI: 10.1016/j.jid.2023.03.1664.

Baugh, S. D.; Morrice, J. R.; Reitz, A. B.; Shaw, C. A.; Gregory-Evans, C. Y. Levamisole derivatives as immune modulators for the treatment of amyotrophic lateral sclerosis (ALS). Future Med. Chem. 2023, 15, DOI: 10.4155/fmc-2023-0028.

Wiah, S.; Roger, A.; Zhao, P.; Shekarabi, A.; Watson, M. N.; Farkas, D. J.; Potula, R.; Reitz, A. B.; Rawls, S. M. Troriluzole inhibits methamphetamine place preference in rats and normalizes methamphetamine-evoked glutamate carboxypeptidase II (GCPII) protein levels in the mesolimbic pathway. Drug Alcohol Depend., 2023, 242:109719.

Guan, H.; Nuth, M.; Isaacs, S. N.; Xiao, Y.; Scott, R.; Parker, M. H.; Strobel, E. D. Kulp, J. L. III; Bailey, T. R.; Reitz, A. B.; Ricciardi, R. P. A small molecule that targets the processivity factor of molluscum contagiosum virus has therapeutic potential. Antiviral Research, 2023, 211, 105520.

Simmons, S. J.; Oliver, C. F.; McCloskey, N. S.; Reitz, A. B.; Nayak, S. U.; Watson, M. N.; Rawls, S. M. Paradoxical anxiolytic effect of the ‘bath salt’ synthetic cathinone MDPV during early abstinence is inhibited by a chemokine CXCR4 or CCR5 receptor antagonist. Drug Alcohol Depend. 2022, 230:109204.  doi: 10.1016/j.drugalcdep.2021.109204.

Baugh, S. D. P.; Jackson, M. R.; Rashad, A. A. Reitz, A. B.; Lam, P. Y. S.; Jorns, M. S. Synthesis and evaluation of potent novel inhibitors of human sulfide:quinone oxidoreductase. Bioorg. Med. Chem. Lett. 2021, 54:128443.  doi: 10.1016/j.bmcl.2021.128443.

Baugh, S. D. P.; Chaly, A.; Weaver, D. G.; Pelletier, J. C.; Thanna, S.; Freeman, K. B.; Reitz, A. B.; Scott, R. W. Highly potent, broadly active antifungal agents for the treatment of invasive fungal infections. Bioorg. Med. Chem. Lett. 2021, Feb, 1;33.127727. doi:10.1016/j.bmcl.2020.127727

Guan, H.; Nuth, M.; Lee, V.; Lin, C.; Mitchell, C. H.; Lu, W.; Scott, R. W.; Parker, M. H.; Kulp, J. L., Jr.; Reitz, A. B.; Ricciardi, R. P. Herpes Simplex Virus-1 infection in human primary corneal epithelial cells is blocked by a stapled peptide that targets processive DNA synthesis. Ocul. Surf. 2021, 19 , 313-321.

Han, Z.; Ye, H.; Liang, J.; Shepley-McTaggart, A.; Wrobel, J. E.; Reitz, A. B.; Whigham, A.; Kavelish, K. N.; Saporito, M. S.; Freedman, B. D.; Shtanko, O.; Harty, R. N. Compound FC-10696 Inhibits Egress of Marburg Virus. Antimicrob. Agents Chemother. 2021, doi: 10.1128/AAC.00086-21 (online ahead of print).

Messick, T. E.; Tolvinski, L.; Zartler, E. R.; Moberg, A.; Frostell, A.; Smith, G. R.; Reitz, A. B.; Lieberman, P. M. Biophysical Screens Identify Fragments that Bind to the Viral DNA-Binding Proteins EBNA1 and LANA. Molecules. 2020, 25 , 1760.

Robinson, R. M.; Reyes, L.; Duncan, R. M.; Bian, H.; Strobel, E. D.; Hyman, S. L.; Reitz, A. B.; Dolloff, N. G. Tuning isoform selectivity and bortezomib sensitivity with a new class of alkenyl indene PDI inhibitor. Eur. J. Med. Chem. 2020, 186 , 111906.

Shi, H.; Tice, C. M.; Emert-Sedlak, L.; Chen, L.; Li, W. F.; Carlsen, M.; Wrobel, J. E.; Reitz, A. B.; Smithgall, T. E. Tight-Binding Hydroxypyrazole NIV-1 Nef Inhibitors Suppress Viral Replication in Donor Mononuclear Cells and Reverse Nef-Mediated MHC-1 Downregulation. ACS Infectious Diseases 2020, 6, 302-312.

Punchi Hewage, A. N. D.; Yao, H.; Nammalwar, B. Gnanasekaran, K. K.; Lovell, S.; Bunce, R. A.; Eshelman, K.; Phaniraj, S. M.; Lee, M. M.; Peterson, B. R.; Battaile, K. P.; Reitz, A. B.; Rivera, M. Small Molecule Inhibitors of the BfrB-Bfd Interaction Decrease Pseudomonas aeruginona Fitness and Potentiate Fluoroquinoline Activity. J. Am. Chem. Soc. 2019, 141, 8171-8184.

Saber, I. Milewski, A.; Reitz, A. B.; Rawls, S. M.; Walker, E. A. Effects of dopaminergic and serotonergic compounds in rats trained to discriminate a high and a low training dose of the synthetic cathinone mephedrone. Psychopharmacology (Berl) 2019, Apr 13. doi: 10.1007/s00213-019-05241-z. [Epub ahead of print].

Karpova, Y.; Wu, C.; Divan, A.; McDonnell, M. E.; Hewlett, E.; Makhov, P.; Gordon, J.; Ye, M.; Reitz, A. B.; Childers, W. E.; Skorski, T.; Kolenko, V.; Tulin, A. V. Non-NAD-like PARP-1 inhibitors in prostate cancer treatment. Biochem. Pharmacol. 2019, 167, 149-162.

Messick, T. E.; Smith, G. R.; Soldan, S. S.; McDonnell, M. E.; Deakyne, J. S.; Malecka, K. A.; Tolvinski, L.; van den Heuvel, A. P. J.; Gu, B. W.; Cassel, J. A.; Tran, D. H.; Wasserman, B. R.; Zhang, Y.; Velvadapu, V.; Zartler, E. R.; Busson, P.; Reitz, A. B.; Lieberman, P. M. Structure-based design of small-molecule inhibitors of EBNA1 DNA binding blocks Epstein-Barr virus latent infection and tumor growth. Sci. Tranl. Med. 2019, 11 , pii: eaau5612. doi: 10.1126/scitranslmed.aau5612.

Gentile, T. A.; Simmons, S. J.; Tallarida, C. S.; Su, S.; Rom, S.; Watson, M. N.; Reitz, A. B.; Potula, R.; Rawls, S. M. Synthetic cathinone MDPV enhances reward function through purinergic P2X7 receptor-dependent pathway and increases P2X7 gene expression in nucleus accumbens. Drug Alcohol Depend. 2019, 197 , 22-27.

Nuth, M.; Guan, H.; Xiao, Y.; Kulp, J. L., 3rd; Parker, M. H.; Strobel, E. D.; Issacs, S. N.; Scott, R. W.; Reitz, A. B.; Ricciardi, R. P. Mutation and structure guided discovery of an antiviral small molecule that mimics an essential C-terminal tripeptide of the vaccinia D4 processivity factor. Antiviral Res. 2019, 162 , 178-185.

Selwood, T.; Larsen, B. J.; Mo, C. Y.; Culyba, M. J.; Hostetler, Z. M.; Kohli, R. M.; Reitz, A. B.; Baugh, S. D. P. Advancement of the 5-Amino-1-(Carbamoylmethyl)-1H-1,2,3-Trazole-4-Carboxamide Scaffold to Disarm the Bacterial SOS Response. Front. Microbiology. 2018, 9 , 1-11.

Robinson, R. M.; Reyes, L.; Duncan, R. M.; Bian, H.; Reitz, A. B.; Manevich, Y.; McClure, J. J.; Champion, M. M.; Chou, C. J.; Sharik, M. E.; Chesi, M.; Bergsagel, P. L.; Dolloff, N. G. Inhibitors of the protein disulfide isomerase family for the treatment of multiple myeloma. Leukemia. 2018, Oct 12. doi: 10.1038/s41375-018-0263-1. [Epub ahead of print]

Pelletier J. C.; Chen, S.; Bian, H.; Shah, R.; Smith, G. R.; Wrobel, J. E.; Reitz, A. B. Dipeptide Prodrugs of the Glutamate Modulator Riluzole. ACS Med. Chem. Lett. 2018, 9 , 752-756.

Swiatkowski, P.; Sewell, E.; Sweet, E. S.; Dickson, S.; Swanson, R. A.; McEwan, S. A.; Cuccolo, N.; McDonnell, M. E.; Patel, M. V.; Varghese, N.; Morrison, B.; Reitz, A. B.; Meaney, D. F.; Firestein, B. L. Cypin: A novel target for traumatic brain injury. Neurobiol. Dis. 2018, 119 , 13-25.

Larsen, B. J.; Rosano, R. J.; Ford-Hutchinson, T. A.; Reitz, A. B.; Wrobel, J. A. A method for C2 arylation of 1,3-indandiones. Tetrahedron. 2018, 74 , 2762-2768.

Hicks, C.; Huang, P.; Ramos, L.; Nayak, S. U.; Caro, Y.; Reitz, A. B.; Smith, G. R.; Lee, D. Y.; Rawls, S. M.; Liu-Chen, L. Y. Dopamine D1-Like Receptor Agonist and D2-Like Receptor (-)-Stepholidine Reduces Reinstatement of Drug-Seeking Behavior for 3,4-Methylenedioxypyrovalerone (MDPB) in Rats. ACS Chem. Neurosci. 2018, 9 , 1327-1337.

Oliver C. F.; Simmons, S. J.; Nayak, S. U.; Smith, G. R.; Reitz, A. B.; Rawls, S. M. Chemokines and ‘bath salts’: CXCR4 receptor antagonist reduces rewarding and locomotor stimulant effects of the designer cathinone MDPV in rats. Drug Alcohol Depend. 2018, 186 , 75-79.

Zewde, A. M.; Yu, F.; Nayak, S.; Tallarida, C.; Reitz, A. B.; Kirby, L. G.; Rawls, S. M. PLDT (planarian light/dark test): an invertebrate assay to quantify defensive responding and study anxiety-like effects. J. Neurosci. Methods. 2018, 293 , 284-288.

Hicks, C.; Gregg, R. A.; Nayak, S. U.; Cannella, L. A.; Schena, G. J.; Tallerida, C. S.; Reitz, A. B.; Rawls, S. M. Glutamate carboxypeptidase II (GCPII) inhibitor 2-PMPA reduces rewarding effects of the synthetic cathinone MDPB in rats: a role for N-acetylaspartylglutamate (NAAG). . Psychopharmacology. 2017, 234 , 1671-1681.

Philogene-Khalid, H. L.; Simmons, S. J.; Nayak, S.; Martorana, R. M.; Su, S. H.; Caro, Y.; Ranieri, B.; DiFurio, K.; Mo, L.; Gentile, T. A.; Murad, A.; Reitz, A. B.; Muschamp, J. W.; Rawls, S. M. Stereoselective Differences between the Reinforcing and Motivational Effects of Cathinone-Derived 4-Methylmethcathinone (Mephedrone) in Self-Administering Rats. . ACS Chem. Neurosci. 2017, 8 , 2648-2654.

Philogene-Khalid, H. L.; Hicks, C.; Reitz, A. B.; Liu-Chen, L. Y.; Rawls, S. M. Synthetic cathinones and stereochemistry: S enantiomer of mephedrone reduces anxiety- and depressant-like effects in cocaine- or MDPV-abstinent rats. Drug Alcohol Depend. 2017, 176 , 119-125.

Loughran, H. M.; Han, Z.; Wrobel, J. E.; Decker, S. E.; Ruthel, G.; Freedman, B. D.; Harty, R. N.; Reitzdf, A. B. Quinoxaline-based inhibitors of Ebola and Marburg VP40 egress. Bioorg. Med. Chem. Lett. 2016, 26, 3429-3435.

Gregg, R. A.; Hicks, C.; Nayak, S. U.; Tallarida, C. S.; Nucero, P.; Smith, G. R.; Reitz, A. B.; Rawls, S. M. Synthetic cathinone MDPV downregulates glutamate transporter subtype 1 (GLT-1) and produces rewarding and locomotor-activating effects that are reduced by a GLT-1 activator. Neuropharmacology. 2016, in print (doi: 10.1016/j.neuropharm.2016.04.014. Epub 2016 Apr 13).

Emert-Sedlak, L. A.; Loughran, H. M.; Shi, H.; Kulp, J. L., III; Shu, S. T.; Zhao, J.; Day, B. W.; Wrobel, J. E.; Reitz, A. B.; Smithgall, T. E. Synthesis and evaluation of orally active small molecule HIV-1 Nef antagonists. Bioorg. Med. Chem. Lett. 2016, 26, 1480-1484.

Han, Z.; Madara, J. J.; Herbert, A.; Prugar, L. I.; Ruthel, G.; Lu, J.; Liu, Y.; Liu, W.; Liu, X.; Wrobel, J. E.; Reitz, A. B.; Dye, J. M.; Harty, R. N.; Freedman, B. D. Calcium Regulation of Hemorrhagic Fever Virus Budding: Mechanistic Implications for Host-Oriented Therapeutic Intervention. PLoS Pathog. 2015, 11 , e1005220.

Gregg, R. A.; Baumann, M. H.; Partilla, J. S.; Bonano, J. S.; Vouga, A.; Tallarida, C. S.; Velvadapu, V.; Smith, G. R.; Peet, M. M.; Reitz, A. B.; Negus, S. S.; Rawls, S. M. Stereochemistry of mephedrone neuropharmacology: enantiomer-specific behavioral and neurochemical effects in rats. Br. J. Pharmacol. 2015, 172(3), 883-894.

Martin, M. D.; Calcul, L.; Smith, C.; Jinwal, U. K.; Fontaine, S. N.; Darling, A.; Seeley, K.; Woitas, L.; Narayan, M.; Gestwicki, J. E.; Smith, G. R.; Reitz, A. B.; Baker, B. J.; Dickey, C. A. Synthesis, Stereochemical Analysis, and Derivatization of Myricanol Provide New Probes That Promote Autophagic Tau Clearance. ACS Chem. Biol 2015, 10, 1099-1109.

Vouga, A.; Gregg, R. A.; Haidery, M.; Ramnath, A.; Al-Hassani, H. K.; Tallarida, C. S.; Grizzanti, D.; Raffa, R. B.; Smith, G. R.; Reitz, A. B.; Rawls, S. M. Stereochemistry and neuropharmacology of a ‘bath salt’ cathinone: S-enantiomer of mephedrone reduces cocaine-induced reward and withdrawal in invertebrates. Neuropharmacology 2015, 91, 109-16.

Rubin, H.; Selwood, T.; Yano, T.; Weaver, D. G.; Loughran, H. M.; Costanzo, M. J.; Scott, R. W.; Wrobel, J. E.; Freeman, K. B.; Reitz, A. B. Acinetobacter baumannii OxPhos inhibitors as selective anti-infective agents. Bioorg. Med. Chem. Lett. 2015, 25, 378-383.

Pelletier, J. C.; Velvadapu, V.; McDonnell, M. E.; Wrobel, J. E.; Reitz, A. B. Intramolecular rearrangement of α-amino acid amide derivatives of 2-aminobenzothiazoles. Tetrahedron Lett. 2014, 55, 4193-4195.

Han, Z.; Lu, J.; Liu, Y.; Davis, B.; Lee, M. S.; Olson, M. A.; Ruthel, G.; Freedman, B. D.; Schnell, M. J.; Wrobel, J. E.; Reitz, A. B.; and Harty, R. N. Small Molecule Probes Targeting the Viral PPxY-Host Nedd4 Interface Block Egress of a Broad Range of RNA Viruses. Journal of Virology, 2014, 88, 7294-7306.

McDonnell, M. E.; Bian, H.;Wrobel, J.; Smith, G. R.; Liang, S.; Ma, H.; Reitz, A. B. Anilino-monoindolylmaleimides as potent and selective JAK3 inhibitors. Bioorg Med Chem Lett. 2014, 24, 1116-1121.

Caglic, D.; Krutein, M. C.; Bompiani, K. M.; Barlow, D. J.; Benomi, G.; Pelletier, J. C.; Reitz, A. B.; Lairson, L. L.; Houseknecht, K. L.; Smith, G. R.; Dickerson, T. J. Identification of clinically viable quinolinol inhibitors of botulinum neurotoxin A light chain. J. Med. Chem. 2014, 57, 669-676.

Smith, G. R.; Brenneman, D. E.; Zhang, Y.; Du, Y.; Reitz, A. B. Small-Molecule Anticonvulsant Agents with Potent In Vitro Neuroprotection and Favorable Drug-Like Properties. J. Mol. Neurosci. 2014, 52, 446-458.

Gregg, R. A.; Tallarida, C. S.; Reitz, A. B.; McCurdy, C.; Rawls, S. M. Mephedron (4-methylmethcathinone), a principal constituent of psychoactive bath salts, produces behavioral sensitization in rats. Drug Alcohol Depend. 2013, 133, 746-750.

Gregg, R. A.; Tallarida, C. S.; Reitz, A. B.; Rawls, S. M. Mephedrone interactions with cocaine: prior exposure to the ‘bath salt’ constituent enhances cocaine-induced locomotor activation in rats. Behavioural Pharmacology 2013, 24, 684-688.

Watterson, D. M.; Grum-Tokars, V. L.; Roy, S. M.; Schavocky, J. P.; Bradaric, B. D.; Bachstetter, A. D.; Xing, B.; Dimayuga, E.; Saeed, F.; Zhang, H.; Staniszewski, A.; Pelletier, J. C.; Minasov, G.; Anderson, W. F.; Arancio, O.; Van Eldick, L. J. Development of Novel In Vivo Chemical Probes to Address CNS Protein Kinase Involvement in Synaptic Dysfunction. PLoS ONE 2013, 8(6), e66226.

Ramoz, L.; Lodi, S.; Bhatt, P.; Reitz, A. B.; Tallarida, C.; Tallarida, R. J.; Raffa, R. B.; Rawls, S. M. Mephedrone (‘Bath Salt’) Pharmacology: Insights from Invertebrates, Neuroscience, 2012, 208, 79-84.

Lisek, R.; Yuvasheva, E.; Chiu, Y. T.; Reitz, A. B.; Liu-Chen, L. Y.; Rawls, S. M. Mephedrone (‘Bath Salt’) Elicits Conditioned Place Preference and Dopamine-Sensitive Locomotor-Sensitive Activation. Drug and Alcohol Dependence, 2012, 126, 257-262.

Cassel, J. A.; Ilyin, S.; McDonnell, M. E.; Reitz, A. B. Novel Inhibitors of Heat Shock Protein Hsp70-Mediated Luciferase Refolding that Bind to DnaJ, Bioorg. Med. Chem. Lett. 2012, 20, 3609-3614.

Cassel, J. A.; McDonnell, M. E.; Velvadapu, V.; Andrianov, V.; Reitz, A. B. The effects of small molecule inhibitors of nucleic acid binding to TDP-43 on TDP-43 metabolism and function. Biochimie, 2012, 94, 1974-1981.

Smith, G. R.; Caglič, D.; Čapek, P.; Zhang, Y.; Godbole, S.; Reitz, A. B.; Dickerson, T. J. Reexamining hydroxamate inhibitors of Botulinum neurotoxin serotype A: Extending towards the b-exosite. Bioorg. Med. Chem. Lett. 2012, 22, 3754-3757.

McDonnell, M. E.; Vera, M. D.; Blass, B. E.; Pelletier, J. C.; King, R. C.; Fernandez-Metzler, C.; Smith, G. R.; Wrobel, J.; Chen, S.; Reitz, A. B. Riluzole prodrugs for melanoma and ALS: design, synthesis, and in vitro metabolic profiling. 2012, Bioorg. Med. Chem., 20, 5642-5648.

Velvadapu, V., McDonnell, M. E., Jaffe, E. K., Reitz, A. B.  Facile Synthesis of Mutagen X (MX): 3-Chloro-4-(dichloromethyl)-5-hydroxy-5H-furan-2-one. Tetrahedron Letters, 2012, 53, 3144-3146.

Brenneman, D. E.; Smith, G. R.; Zhang, Y.; Du, Y.; Kondaveeti, S. K.; Zdilla, M. J.; Reitz, A. B.  Small-Molecule Anticonvulsant Agents with Potent in vitro Neuroprotection. J. Molecular Neuroscience, 2012, 47, 368-379.

Venkatesh, M., Wang, H., Cayer, J., Leroux, M., Salvail, D., Das, B., Wrobel, J., Mani, S. In Vivo and In Vitro Characterization of a Frist-in-Class Novel Azole Analog That Targets Pregnane X Receptor Activation. Molecular Pharmacology, 2011, 80, 124-135.

Čapek, P., Zhang, Y., Barlow, D.J., Houseknecht, K.L., Smith, G., Dickerson, T.J. Enhancing the Pharmacokinetic Properties of Botulinum Neurotoxin Serotype A Protease Inhibitors through Rational Design. ACS Chemical Neuroscience, 2011, 2, 288-293.

Reitz, A. B.; Ramirez, U. D.; Stith, L.; Du, Y.; Smith, G. R.; Jaffe, E. K. Pseudomonas aeruginosa Porphobilinogen Synthase Assembly State Regulators: Hit Discovery and Initial SAR Studies. ARKIVOC, 2010, 175-188.

Reitz, A. B.; Smith, G. R.; Tounge, B. A.; Reynolds, C. H. Hit Triage Using Efficiency Indices after Screening of Compound Libraries in Drug Discovery. Curr. Top. Med. Chem., 2009, 9, 1718-1724.

Close
Q

There is no guarantee in drug discovery but we seek to improve the odds so we have a greater chance of success.

Allen Reitz, Ph.D., CEO

DOCUMENTS

PUBLICATIONS

Guan H, Nuth M, Scott RW, Parker MH, Strobel ED, Reitz AB, Kulp JL 3rd, Ricciardi RP. Potency of a small molecule that targets the molluscum contagiosum virus processivity factor increases when conjugated to a tripeptide. Antiviral Res. 2024 Jun;226:105899. doi: 10.1016/j.antiviral.2024.105899.

Eddy K, Gupta K, Eddin MN, Marinaro C, Putta S, Sauer JM Jr, Chaly A, Freeman KB, Pelletier JC, Fateeva A, Furmanski P, Silk AW, Reitz AB, Zloza A, Chen S. Assessing Longitudinal Treatment Efficacies and Alterations in Molecular Markers Associated with Glutamatergic Signaling and Immune Checkpoint Inhibitors in a Spontaneous Melanoma Mouse Model. JID Innov. 2024 Jan 18;4(2):100262. doi: 10.1016/j.xjidi.2024.100262.

Shields BC, Yan H, Lim SSX, Burwell SCV, Cammarata CM, Fleming EA, Yousefzadeh SA, Goldenshtein VZ, Kahuno EW, Vagadia PP, Loughran MH, Zhiquan L, McDonnell ME, Scalabrino ML, Thapa M, Hawley TM, Field GD, Hull C, Schiltz GE, Glickfeld LL, Reitz AB, Tadross MR. DART.2: bidirectional synaptic pharmacology with thousandfold cellular specificity. Nat Methods. 2024 Jul;21(7):1288-1297. doi: 10.1038/s41592-024-02292-9.

Emert-Sediak, L. A.; Tice, C. M.; Shi, H.; Alvarado, J. J.; Shu, S. T.; Reitz, A. B.; Smithgall, T. E. PROTAC-mediated degradation of HIV-1 Nef efficiently restores cell-surface CD4 and MHC-I expression and blocks HIV-1 replication. Cell Chem. Biol. 2024, 31, 1-11. doi:10.1016/j.chembiol.2024.02.004.

Eddy, K.; Gupta, K.; Pelletier, J. C.; Isola, A. L.; Marinaro, C.; Rasheed, M. A.; Campagnolo, J.; Eddin, M. N.; Rossi, N.; Fateeva, A.; Reuhl,, K.; Shah, R.; Robinson, A. K.; Chaly, A.; Freeman, K. B.; Chen, W.; Diaz, J.; Furmanski, P.; Silk, A. W.; Reitz, A. B.; Zloza, A.; Chen. S. A Spontaneous Melanoma Mouse Model Applicable for a longitudinal Chemotherapy and Immunotherapy Study. J. Investigative Dermatology, 2023, 143, 2007-2018. DOI: 10.1016/j.jid.2023.03.1664

LIST OF SELECTED PUBLICATIONS

SELECTED PUBLICATIONS

Emert-Sediak, L. A.; Tice, C. M.; Shi, H.; Alvarado, J. J.; Shu, S. T.; Reitz, A. B.; Smithgall, T. E. PROTAC-mediated degradation of HIV-1 Nef efficiently restores cell-surface CD4 and MHC-I expression and blocks HIV-1 replication. Cell Chem. Biol. 2024, 31, 1-11. doi:10.1016/j.chembiol.2024.02.004.

Eddy, K.; Gupta, K.; Pelletier, J. C.; Isola, A. L.; Marinaro, C.; Rasheed, M. A.; Campagnolo, J.; Eddin, M. N.; Rossi, N.; Fateeva, A.; Reuhl,, K.; Shah, R.; Robinson, A. K.; Chaly, A.; Freeman, K. B.; Chen, W.; Diaz, J.; Furmanski, P.; Silk, A. W.; Reitz, A. B.; Zloza, A.; Chen. S. A Spontaneous Melanoma Mouse Model Applicable for a longitudinal Chemotherapy and Immunotherapy Study. J. Investigative Dermatology, 2023, 143, 2007-2018. DOI: 10.1016/j.jid.2023.03.1664.

Baugh, S. D.; Morrice, J. R.; Reitz, A. B.; Shaw, C. A.; Gregory-Evans, C. Y. Levamisole derivatives as immune modulators for the treatment of amyotrophic lateral sclerosis (ALS). Future Med. Chem. 2023, 15, DOI: 10.4155/fmc-2023-0028.

Wiah, S.; Roger, A.; Zhao, P.; Shekarabi, A.; Watson, M. N.; Farkas, D. J.; Potula, R.; Reitz, A. B.; Rawls, S. M. Troriluzole inhibits methamphetamine place preference in rats and normalizes methamphetamine-evoked glutamate carboxypeptidase II (GCPII) protein levels in the mesolimbic pathway. Drug Alcohol Depend., 2023, 242:109719.

Guan, H.; Nuth, M.; Isaacs, S. N.; Xiao, Y.; Scott, R.; Parker, M. H.; Strobel, E. D. Kulp, J. L. III; Bailey, T. R.; Reitz, A. B.; Ricciardi, R. P. A small molecule that targets the processivity factor of molluscum contagiosum virus has therapeutic potential. Antiviral Research, 2023, 211, 105520.

Simmons, S. J.; Oliver, C. F.; McCloskey, N. S.; Reitz, A. B.; Nayak, S. U.; Watson, M. N.; Rawls, S. M. Paradoxical anxiolytic effect of the ‘bath salt’ synthetic cathinone MDPV during early abstinence is inhibited by a chemokine CXCR4 or CCR5 receptor antagonist. Drug Alcohol Depend. 2022, 230:109204.  doi: 10.1016/j.drugalcdep.2021.109204.

Baugh, S. D. P.; Jackson, M. R.; Rashad, A. A. Reitz, A. B.; Lam, P. Y. S.; Jorns, M. S. Synthesis and evaluation of potent novel inhibitors of human sulfide:quinone oxidoreductase. Bioorg. Med. Chem. Lett. 2021, 54:128443.  doi: 10.1016/j.bmcl.2021.128443.

Baugh, S. D. P.; Chaly, A.; Weaver, D. G.; Pelletier, J. C.; Thanna, S.; Freeman, K. B.; Reitz, A. B.; Scott, R. W. Highly potent, broadly active antifungal agents for the treatment of invasive fungal infections. Bioorg. Med. Chem. Lett. 2021, Feb, 1;33.127727. doi:10.1016/j.bmcl.2020.127727

Guan, H.; Nuth, M.; Lee, V.; Lin, C.; Mitchell, C. H.; Lu, W.; Scott, R. W.; Parker, M. H.; Kulp, J. L., Jr.; Reitz, A. B.; Ricciardi, R. P. Herpes Simplex Virus-1 infection in human primary corneal epithelial cells is blocked by a stapled peptide that targets processive DNA synthesis. Ocul. Surf. 2021, 19 , 313-321.

Han, Z.; Ye, H.; Liang, J.; Shepley-McTaggart, A.; Wrobel, J. E.; Reitz, A. B.; Whigham, A.; Kavelish, K. N.; Saporito, M. S.; Freedman, B. D.; Shtanko, O.; Harty, R. N. Compound FC-10696 Inhibits Egress of Marburg Virus. Antimicrob. Agents Chemother. 2021, doi: 10.1128/AAC.00086-21 (online ahead of print).

Messick, T. E.; Tolvinski, L.; Zartler, E. R.; Moberg, A.; Frostell, A.; Smith, G. R.; Reitz, A. B.; Lieberman, P. M. Biophysical Screens Identify Fragments that Bind to the Viral DNA-Binding Proteins EBNA1 and LANA. Molecules. 2020, 25 , 1760.

Robinson, R. M.; Reyes, L.; Duncan, R. M.; Bian, H.; Strobel, E. D.; Hyman, S. L.; Reitz, A. B.; Dolloff, N. G. Tuning isoform selectivity and bortezomib sensitivity with a new class of alkenyl indene PDI inhibitor. Eur. J. Med. Chem. 2020, 186 , 111906.

Shi, H.; Tice, C. M.; Emert-Sedlak, L.; Chen, L.; Li, W. F.; Carlsen, M.; Wrobel, J. E.; Reitz, A. B.; Smithgall, T. E. Tight-Binding Hydroxypyrazole NIV-1 Nef Inhibitors Suppress Viral Replication in Donor Mononuclear Cells and Reverse Nef-Mediated MHC-1 Downregulation. ACS Infectious Diseases 2020, 6, 302-312.

Punchi Hewage, A. N. D.; Yao, H.; Nammalwar, B. Gnanasekaran, K. K.; Lovell, S.; Bunce, R. A.; Eshelman, K.; Phaniraj, S. M.; Lee, M. M.; Peterson, B. R.; Battaile, K. P.; Reitz, A. B.; Rivera, M. Small Molecule Inhibitors of the BfrB-Bfd Interaction Decrease Pseudomonas aeruginona Fitness and Potentiate Fluoroquinoline Activity. J. Am. Chem. Soc. 2019, 141, 8171-8184.

Saber, I. Milewski, A.; Reitz, A. B.; Rawls, S. M.; Walker, E. A. Effects of dopaminergic and serotonergic compounds in rats trained to discriminate a high and a low training dose of the synthetic cathinone mephedrone. Psychopharmacology (Berl) 2019, Apr 13. doi: 10.1007/s00213-019-05241-z. [Epub ahead of print].

Karpova, Y.; Wu, C.; Divan, A.; McDonnell, M. E.; Hewlett, E.; Makhov, P.; Gordon, J.; Ye, M.; Reitz, A. B.; Childers, W. E.; Skorski, T.; Kolenko, V.; Tulin, A. V. Non-NAD-like PARP-1 inhibitors in prostate cancer treatment. Biochem. Pharmacol. 2019, 167, 149-162.

Messick, T. E.; Smith, G. R.; Soldan, S. S.; McDonnell, M. E.; Deakyne, J. S.; Malecka, K. A.; Tolvinski, L.; van den Heuvel, A. P. J.; Gu, B. W.; Cassel, J. A.; Tran, D. H.; Wasserman, B. R.; Zhang, Y.; Velvadapu, V.; Zartler, E. R.; Busson, P.; Reitz, A. B.; Lieberman, P. M. Structure-based design of small-molecule inhibitors of EBNA1 DNA binding blocks Epstein-Barr virus latent infection and tumor growth. Sci. Tranl. Med. 2019, 11 , pii: eaau5612. doi: 10.1126/scitranslmed.aau5612.

Gentile, T. A.; Simmons, S. J.; Tallarida, C. S.; Su, S.; Rom, S.; Watson, M. N.; Reitz, A. B.; Potula, R.; Rawls, S. M. Synthetic cathinone MDPV enhances reward function through purinergic P2X7 receptor-dependent pathway and increases P2X7 gene expression in nucleus accumbens. Drug Alcohol Depend. 2019, 197 , 22-27.

Nuth, M.; Guan, H.; Xiao, Y.; Kulp, J. L., 3rd; Parker, M. H.; Strobel, E. D.; Issacs, S. N.; Scott, R. W.; Reitz, A. B.; Ricciardi, R. P. Mutation and structure guided discovery of an antiviral small molecule that mimics an essential C-terminal tripeptide of the vaccinia D4 processivity factor. Antiviral Res. 2019, 162 , 178-185.

Selwood, T.; Larsen, B. J.; Mo, C. Y.; Culyba, M. J.; Hostetler, Z. M.; Kohli, R. M.; Reitz, A. B.; Baugh, S. D. P. Advancement of the 5-Amino-1-(Carbamoylmethyl)-1H-1,2,3-Trazole-4-Carboxamide Scaffold to Disarm the Bacterial SOS Response. Front. Microbiology. 2018, 9 , 1-11.

Robinson, R. M.; Reyes, L.; Duncan, R. M.; Bian, H.; Reitz, A. B.; Manevich, Y.; McClure, J. J.; Champion, M. M.; Chou, C. J.; Sharik, M. E.; Chesi, M.; Bergsagel, P. L.; Dolloff, N. G. Inhibitors of the protein disulfide isomerase family for the treatment of multiple myeloma. Leukemia. 2018, Oct 12. doi: 10.1038/s41375-018-0263-1. [Epub ahead of print]

Pelletier J. C.; Chen, S.; Bian, H.; Shah, R.; Smith, G. R.; Wrobel, J. E.; Reitz, A. B. Dipeptide Prodrugs of the Glutamate Modulator Riluzole. ACS Med. Chem. Lett. 2018, 9 , 752-756.

Swiatkowski, P.; Sewell, E.; Sweet, E. S.; Dickson, S.; Swanson, R. A.; McEwan, S. A.; Cuccolo, N.; McDonnell, M. E.; Patel, M. V.; Varghese, N.; Morrison, B.; Reitz, A. B.; Meaney, D. F.; Firestein, B. L. Cypin: A novel target for traumatic brain injury. Neurobiol. Dis. 2018, 119 , 13-25.

Larsen, B. J.; Rosano, R. J.; Ford-Hutchinson, T. A.; Reitz, A. B.; Wrobel, J. A. A method for C2 arylation of 1,3-indandiones. Tetrahedron. 2018, 74 , 2762-2768.

Hicks, C.; Huang, P.; Ramos, L.; Nayak, S. U.; Caro, Y.; Reitz, A. B.; Smith, G. R.; Lee, D. Y.; Rawls, S. M.; Liu-Chen, L. Y. Dopamine D1-Like Receptor Agonist and D2-Like Receptor (-)-Stepholidine Reduces Reinstatement of Drug-Seeking Behavior for 3,4-Methylenedioxypyrovalerone (MDPB) in Rats. ACS Chem. Neurosci. 2018, 9 , 1327-1337.

Oliver C. F.; Simmons, S. J.; Nayak, S. U.; Smith, G. R.; Reitz, A. B.; Rawls, S. M. Chemokines and ‘bath salts’: CXCR4 receptor antagonist reduces rewarding and locomotor stimulant effects of the designer cathinone MDPV in rats. Drug Alcohol Depend. 2018, 186 , 75-79.

Zewde, A. M.; Yu, F.; Nayak, S.; Tallarida, C.; Reitz, A. B.; Kirby, L. G.; Rawls, S. M. PLDT (planarian light/dark test): an invertebrate assay to quantify defensive responding and study anxiety-like effects. J. Neurosci. Methods. 2018, 293 , 284-288.

Hicks, C.; Gregg, R. A.; Nayak, S. U.; Cannella, L. A.; Schena, G. J.; Tallerida, C. S.; Reitz, A. B.; Rawls, S. M. Glutamate carboxypeptidase II (GCPII) inhibitor 2-PMPA reduces rewarding effects of the synthetic cathinone MDPB in rats: a role for N-acetylaspartylglutamate (NAAG). . Psychopharmacology. 2017, 234 , 1671-1681.

Philogene-Khalid, H. L.; Simmons, S. J.; Nayak, S.; Martorana, R. M.; Su, S. H.; Caro, Y.; Ranieri, B.; DiFurio, K.; Mo, L.; Gentile, T. A.; Murad, A.; Reitz, A. B.; Muschamp, J. W.; Rawls, S. M. Stereoselective Differences between the Reinforcing and Motivational Effects of Cathinone-Derived 4-Methylmethcathinone (Mephedrone) in Self-Administering Rats. . ACS Chem. Neurosci. 2017, 8 , 2648-2654.

Philogene-Khalid, H. L.; Hicks, C.; Reitz, A. B.; Liu-Chen, L. Y.; Rawls, S. M. Synthetic cathinones and stereochemistry: S enantiomer of mephedrone reduces anxiety- and depressant-like effects in cocaine- or MDPV-abstinent rats. Drug Alcohol Depend. 2017, 176 , 119-125.

Loughran, H. M.; Han, Z.; Wrobel, J. E.; Decker, S. E.; Ruthel, G.; Freedman, B. D.; Harty, R. N.; Reitzdf, A. B. Quinoxaline-based inhibitors of Ebola and Marburg VP40 egress. Bioorg. Med. Chem. Lett. 2016, 26, 3429-3435.

Gregg, R. A.; Hicks, C.; Nayak, S. U.; Tallarida, C. S.; Nucero, P.; Smith, G. R.; Reitz, A. B.; Rawls, S. M. Synthetic cathinone MDPV downregulates glutamate transporter subtype 1 (GLT-1) and produces rewarding and locomotor-activating effects that are reduced by a GLT-1 activator. Neuropharmacology. 2016, in print (doi: 10.1016/j.neuropharm.2016.04.014. Epub 2016 Apr 13).

Emert-Sedlak, L. A.; Loughran, H. M.; Shi, H.; Kulp, J. L., III; Shu, S. T.; Zhao, J.; Day, B. W.; Wrobel, J. E.; Reitz, A. B.; Smithgall, T. E. Synthesis and evaluation of orally active small molecule HIV-1 Nef antagonists. Bioorg. Med. Chem. Lett. 2016, 26, 1480-1484.

Han, Z.; Madara, J. J.; Herbert, A.; Prugar, L. I.; Ruthel, G.; Lu, J.; Liu, Y.; Liu, W.; Liu, X.; Wrobel, J. E.; Reitz, A. B.; Dye, J. M.; Harty, R. N.; Freedman, B. D. Calcium Regulation of Hemorrhagic Fever Virus Budding: Mechanistic Implications for Host-Oriented Therapeutic Intervention. PLoS Pathog. 2015, 11 , e1005220.

Gregg, R. A.; Baumann, M. H.; Partilla, J. S.; Bonano, J. S.; Vouga, A.; Tallarida, C. S.; Velvadapu, V.; Smith, G. R.; Peet, M. M.; Reitz, A. B.; Negus, S. S.; Rawls, S. M. Stereochemistry of mephedrone neuropharmacology: enantiomer-specific behavioral and neurochemical effects in rats. Br. J. Pharmacol. 2015, 172(3), 883-894.

Martin, M. D.; Calcul, L.; Smith, C.; Jinwal, U. K.; Fontaine, S. N.; Darling, A.; Seeley, K.; Woitas, L.; Narayan, M.; Gestwicki, J. E.; Smith, G. R.; Reitz, A. B.; Baker, B. J.; Dickey, C. A. Synthesis, Stereochemical Analysis, and Derivatization of Myricanol Provide New Probes That Promote Autophagic Tau Clearance. ACS Chem. Biol 2015, 10, 1099-1109.

Vouga, A.; Gregg, R. A.; Haidery, M.; Ramnath, A.; Al-Hassani, H. K.; Tallarida, C. S.; Grizzanti, D.; Raffa, R. B.; Smith, G. R.; Reitz, A. B.; Rawls, S. M. Stereochemistry and neuropharmacology of a ‘bath salt’ cathinone: S-enantiomer of mephedrone reduces cocaine-induced reward and withdrawal in invertebrates. Neuropharmacology 2015, 91, 109-16.

Rubin, H.; Selwood, T.; Yano, T.; Weaver, D. G.; Loughran, H. M.; Costanzo, M. J.; Scott, R. W.; Wrobel, J. E.; Freeman, K. B.; Reitz, A. B. Acinetobacter baumannii OxPhos inhibitors as selective anti-infective agents. Bioorg. Med. Chem. Lett. 2015, 25, 378-383.

Pelletier, J. C.; Velvadapu, V.; McDonnell, M. E.; Wrobel, J. E.; Reitz, A. B. Intramolecular rearrangement of α-amino acid amide derivatives of 2-aminobenzothiazoles. Tetrahedron Lett. 2014, 55, 4193-4195.

Han, Z.; Lu, J.; Liu, Y.; Davis, B.; Lee, M. S.; Olson, M. A.; Ruthel, G.; Freedman, B. D.; Schnell, M. J.; Wrobel, J. E.; Reitz, A. B.; and Harty, R. N. Small Molecule Probes Targeting the Viral PPxY-Host Nedd4 Interface Block Egress of a Broad Range of RNA Viruses. Journal of Virology, 2014, 88, 7294-7306.

McDonnell, M. E.; Bian, H.;Wrobel, J.; Smith, G. R.; Liang, S.; Ma, H.; Reitz, A. B. Anilino-monoindolylmaleimides as potent and selective JAK3 inhibitors. Bioorg Med Chem Lett. 2014, 24, 1116-1121.

Caglic, D.; Krutein, M. C.; Bompiani, K. M.; Barlow, D. J.; Benomi, G.; Pelletier, J. C.; Reitz, A. B.; Lairson, L. L.; Houseknecht, K. L.; Smith, G. R.; Dickerson, T. J. Identification of clinically viable quinolinol inhibitors of botulinum neurotoxin A light chain. J. Med. Chem. 2014, 57, 669-676.

Smith, G. R.; Brenneman, D. E.; Zhang, Y.; Du, Y.; Reitz, A. B. Small-Molecule Anticonvulsant Agents with Potent In Vitro Neuroprotection and Favorable Drug-Like Properties. J. Mol. Neurosci. 2014, 52, 446-458.

Gregg, R. A.; Tallarida, C. S.; Reitz, A. B.; McCurdy, C.; Rawls, S. M. Mephedron (4-methylmethcathinone), a principal constituent of psychoactive bath salts, produces behavioral sensitization in rats. Drug Alcohol Depend. 2013, 133, 746-750.

Gregg, R. A.; Tallarida, C. S.; Reitz, A. B.; Rawls, S. M. Mephedrone interactions with cocaine: prior exposure to the ‘bath salt’ constituent enhances cocaine-induced locomotor activation in rats. Behavioural Pharmacology 2013, 24, 684-688.

Watterson, D. M.; Grum-Tokars, V. L.; Roy, S. M.; Schavocky, J. P.; Bradaric, B. D.; Bachstetter, A. D.; Xing, B.; Dimayuga, E.; Saeed, F.; Zhang, H.; Staniszewski, A.; Pelletier, J. C.; Minasov, G.; Anderson, W. F.; Arancio, O.; Van Eldick, L. J. Development of Novel In Vivo Chemical Probes to Address CNS Protein Kinase Involvement in Synaptic Dysfunction. PLoS ONE 2013, 8(6), e66226.

Ramoz, L.; Lodi, S.; Bhatt, P.; Reitz, A. B.; Tallarida, C.; Tallarida, R. J.; Raffa, R. B.; Rawls, S. M. Mephedrone (‘Bath Salt’) Pharmacology: Insights from Invertebrates, Neuroscience, 2012, 208, 79-84.

Lisek, R.; Yuvasheva, E.; Chiu, Y. T.; Reitz, A. B.; Liu-Chen, L. Y.; Rawls, S. M. Mephedrone (‘Bath Salt’) Elicits Conditioned Place Preference and Dopamine-Sensitive Locomotor-Sensitive Activation. Drug and Alcohol Dependence, 2012, 126, 257-262.

Cassel, J. A.; Ilyin, S.; McDonnell, M. E.; Reitz, A. B. Novel Inhibitors of Heat Shock Protein Hsp70-Mediated Luciferase Refolding that Bind to DnaJ, Bioorg. Med. Chem. Lett. 2012, 20, 3609-3614.

Cassel, J. A.; McDonnell, M. E.; Velvadapu, V.; Andrianov, V.; Reitz, A. B. The effects of small molecule inhibitors of nucleic acid binding to TDP-43 on TDP-43 metabolism and function. Biochimie, 2012, 94, 1974-1981.

Smith, G. R.; Caglič, D.; Čapek, P.; Zhang, Y.; Godbole, S.; Reitz, A. B.; Dickerson, T. J. Reexamining hydroxamate inhibitors of Botulinum neurotoxin serotype A: Extending towards the b-exosite. Bioorg. Med. Chem. Lett. 2012, 22, 3754-3757.

McDonnell, M. E.; Vera, M. D.; Blass, B. E.; Pelletier, J. C.; King, R. C.; Fernandez-Metzler, C.; Smith, G. R.; Wrobel, J.; Chen, S.; Reitz, A. B. Riluzole prodrugs for melanoma and ALS: design, synthesis, and in vitro metabolic profiling. 2012, Bioorg. Med. Chem., 20, 5642-5648.

Velvadapu, V., McDonnell, M. E., Jaffe, E. K., Reitz, A. B.  Facile Synthesis of Mutagen X (MX): 3-Chloro-4-(dichloromethyl)-5-hydroxy-5H-furan-2-one. Tetrahedron Letters, 2012, 53, 3144-3146.

Brenneman, D. E.; Smith, G. R.; Zhang, Y.; Du, Y.; Kondaveeti, S. K.; Zdilla, M. J.; Reitz, A. B.  Small-Molecule Anticonvulsant Agents with Potent in vitro Neuroprotection. J. Molecular Neuroscience, 2012, 47, 368-379.

Venkatesh, M., Wang, H., Cayer, J., Leroux, M., Salvail, D., Das, B., Wrobel, J., Mani, S. In Vivo and In Vitro Characterization of a Frist-in-Class Novel Azole Analog That Targets Pregnane X Receptor Activation. Molecular Pharmacology, 2011, 80, 124-135.

Čapek, P., Zhang, Y., Barlow, D.J., Houseknecht, K.L., Smith, G., Dickerson, T.J. Enhancing the Pharmacokinetic Properties of Botulinum Neurotoxin Serotype A Protease Inhibitors through Rational Design. ACS Chemical Neuroscience, 2011, 2, 288-293.

Reitz, A. B.; Ramirez, U. D.; Stith, L.; Du, Y.; Smith, G. R.; Jaffe, E. K. Pseudomonas aeruginosa Porphobilinogen Synthase Assembly State Regulators: Hit Discovery and Initial SAR Studies. ARKIVOC, 2010, 175-188.

Reitz, A. B.; Smith, G. R.; Tounge, B. A.; Reynolds, C. H. Hit Triage Using Efficiency Indices after Screening of Compound Libraries in Drug Discovery. Curr. Top. Med. Chem., 2009, 9, 1718-1724.

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PUSHING BOUNDARIES OF SCIENTIFIC DISCOVERY

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Phase I STTR Grant

Apr 20, 2021

The Fox Chase Chemical Diversity Center Announces it Has Been Awarded a Phase I STTR Grant...

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PATENTS

Patent No: US 8,609,849 B1
Patent No: US 9,725,427 B2
Patent No: US 9,856,214 B2
Patent No: US 10,112,895 B2
Patent No: US 10,160,756 B2
Patent No: US 10,329,269 B2
Patent No: US 10,357,497 B2
Patent No: US 10,421,718 B2
Patent No: US 10,442,763 B2
Patent No: US 10,485,791 B2
Patent No: US 10,562,870 B2
Patent No: US 10,639,298 B2
Patent No: US 10,780,084 B2
Patent No: US 10,844,026 B2
Patent No: US 10,905,681 B2
Patent No: US 10,981,867 B2
Patent No: US 11,052,070 B2
Patent No: US 11,197,864 B2
Patent No: US 11,242,317 B2
Patent No: US 11,242,338 B2
Patent No: US 11,306,075 B2
Patent No: US 11,440,893 B2
Patent No: US 11,472,776 B2

PATENT DETAILS

ISSUED UNITED STATES PATENTS

US 8,609,849. Hydroxylated Sulfamides Exhibiting Neuroprotective Action and Their Method of Use; with G. R. Smith, D. E. Brenneman, Y. Zhang, and Y. Du (Dec. 17, 2013).

US 9,725,427. Prodrugs of Riluzole and Their Method of Use; with G. R. Smith, M. McDonnell, S. Chen, M. D. Vera, B. E. Blass, J. C. Pelletier, V. N. Velvadapu, and J. E. Wrobel (Aug. 8, 2017).

US 9,856,214. EBNA1 Inhibitors and Their Method of Use; with T. E. Messick, G. R. Smith, P. M. Lieberman, M. E. McDonnell, Y. Zhang, and V. Velvadapu (Jan. 2, 2018)

US 10,112,895. Antivirals Against Molluscum Contagiosum Virus; with P. Ricciardi, M. H. Parker, S. D. P. Baugh, M. Nuth, and H. Guan (Oct. 30, 2018).

US 10,160,756.    Antiviral Compounds and Methods Using Same; with N. Harty, B. D. Freedman, J. E. Wrobel, A. and H. M. Loughran (Dec. 25, 2018).

US 10,329,269. Indene Derivatives and Uses Thereof; with N. G. Dolloff, R. M. Robinson, and H. Baiyan (Jun. 25, 2019).

US 10,357,497.  Pro-Drugs of Riluzole and Their Method of Use for the Treatment of Amyotrophic Lateral Sclerosis; with G. R. Smith (Jul. 23, 2019).

US 10,421,718. EBNA1 Inhibitors and Their Method of Use; with T. E. Messick, G. R. Smith, P. M. Lieberman, M. E. McDonnell, Y. Zhang and V. Velvadapu (Sept. 24, 2019).

US 10,442,763. EBNA1 Inhibitors and Their Method of Use; with T. E. Messick, G. R. Smith, P. M. Lieberman, M. E. McDonnell, Y. Zhang, M. Carlsen, and S. Chen (Oct. 15, 2019).

US 10,485,791. Riluzole Prodrugs and Their Use; with E. Wrobel, J. C. Pelletier, G. R. Smith and Bian (Nov. 26, 2019).

US 10,562,870. Prodrugs of Riluzole and Their Method of Use; with R. Smith, M. McDonnell, Chen, M. D. Vera, B. E. Blass, J. C. Pelletier, V. N. Velvadapu, and J. E. Wrobel (Feb. 18, 2020).

US 10,639,298. Prodrugs of Riluzole and their Method of Use; with R. Smith, H. Bian, J. E. Wrobel and J. C. Pelletier (May 5, 2020).

US 10,780,084. Antibody-Recruiting Molecules for the Treatment of Cancer; with Spiegel, H. Loughran, J. C. Pelletier, and M. E. Welsch (Sept. 22, 2020).

US 10,844,026. Prodrugs of Riluzole and their Method of Use; with G. R. Smith, M. McDonnell, S. Chen, M. D. Vera, B. E. Blass, J. C. Pelletier, V. N. Velvadapu, and J. E. Wrobel (Nov 24, 2020).

US 10,905,681. Riluzole Prodrugs and Their Use; with E. Wrobel, J. C. Pelletier, G. R. Smith, and H. Bian (Feb. 2, 2021).

US 10,981,867. EBNA1 Inhibitors and Methods Using Same; with T. E. Messick, G. R. Smith, P. M. Lieberman, M. E. McDonnell, Y. Zhang, M. Carlsen and S. Chen (Apr. 20, 2021).

US 11,052,070. Riluzole Prodrugs and Their Use; with E. Wrobel, J. C. Pelletier, G. R. Smith and Bian (July 6, 2021).

US 11,197,864. Pro-Drugs of Riluzole and Their Method of Use for the Treatment of Amyotrophic Lateral Sclerosis; with G. R. Smith (Dec. 14, 2021).

US 11,358,935. Prodrugs of Lanicemine and Their Method of Use; with J. C. Pelletier (June 14, 2022).

US 11,472,776. Quinazolines that Inhibit the Formation of Tau Oligomers and their Method of Use; with E. J. Davidowitz, J. G. Moe, H. Bian, C. Glucowski, J. Hendrix, A. S. Yehaskel, M. E. McDonnell, and H. Marie Loughran (Oct. 18, 2022).

Close
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PATENTS

Patent No: US 8,609,849 B1
Patent No: US 9,725,427 B2
Patent No: US 9,856,214 B2
Patent No: US 10,112,895 B2
Patent No: US 10,160,756 B2
Patent No: US 10,329,269 B2
Patent No: US 10,357,497 B2
Patent No: US 10,421,718 B2
Patent No: US 10,442,763 B2
Patent No: US 10,485,791 B2
Patent No: US 10,562,870 B2
Patent No: US 10,639,298 B2
Patent No: US 10,780,084 B2
Patent No: US 10,844,026 B2
Patent No: US 10,905,681 B2
Patent No: US 10,981,867 B2
Patent No: US 11,052,070 B2
Patent No: US 11,197,864 B2
Patent No: US 11,242,317 B2
Patent No: US 11,242,338 B2
Patent No: US 11,306,075 B2
Patent No: US 11,440,893 B2
Patent No: US 11,472,776 B2

PATENT DETAILS

ISSUED UNITED STATES PATENTS

US 8,609,849. Hydroxylated Sulfamides Exhibiting Neuroprotective Action and Their Method of Use; with G. R. Smith, D. E. Brenneman, Y. Zhang, and Y. Du (Dec. 17, 2013).

US 9,725,427. Prodrugs of Riluzole and Their Method of Use; with G. R. Smith, M. McDonnell, S. Chen, M. D. Vera, B. E. Blass, J. C. Pelletier, V. N. Velvadapu, and J. E. Wrobel (Aug. 8, 2017).

US 9,856,214. EBNA1 Inhibitors and Their Method of Use; with T. E. Messick, G. R. Smith, P. M. Lieberman, M. E. McDonnell, Y. Zhang, and V. Velvadapu (Jan. 2, 2018)

US 10,112,895. Antivirals Against Molluscum Contagiosum Virus; with P. Ricciardi, M. H. Parker, S. D. P. Baugh, M. Nuth, and H. Guan (Oct. 30, 2018).

US 10,160,756.    Antiviral Compounds and Methods Using Same; with N. Harty, B. D. Freedman, J. E. Wrobel, A. and H. M. Loughran (Dec. 25, 2018).

US 10,329,269. Indene Derivatives and Uses Thereof; with N. G. Dolloff, R. M. Robinson, and H. Baiyan (Jun. 25, 2019).

US 10,357,497.  Pro-Drugs of Riluzole and Their Method of Use for the Treatment of Amyotrophic Lateral Sclerosis; with G. R. Smith (Jul. 23, 2019).

US 10,421,718. EBNA1 Inhibitors and Their Method of Use; with T. E. Messick, G. R. Smith, P. M. Lieberman, M. E. McDonnell, Y. Zhang and V. Velvadapu (Sept. 24, 2019).

US 10,442,763. EBNA1 Inhibitors and Their Method of Use; with T. E. Messick, G. R. Smith, P. M. Lieberman, M. E. McDonnell, Y. Zhang, M. Carlsen, and S. Chen (Oct. 15, 2019).

US 10,485,791. Riluzole Prodrugs and Their Use; with E. Wrobel, J. C. Pelletier, G. R. Smith and Bian (Nov. 26, 2019).

US 10,562,870. Prodrugs of Riluzole and Their Method of Use; with R. Smith, M. McDonnell, Chen, M. D. Vera, B. E. Blass, J. C. Pelletier, V. N. Velvadapu, and J. E. Wrobel (Feb. 18, 2020).

US 10,639,298. Prodrugs of Riluzole and their Method of Use; with R. Smith, H. Bian, J. E. Wrobel and J. C. Pelletier (May 5, 2020).

US 10,780,084. Antibody-Recruiting Molecules for the Treatment of Cancer; with Spiegel, H. Loughran, J. C. Pelletier, and M. E. Welsch (Sept. 22, 2020).

US 10,844,026. Prodrugs of Riluzole and their Method of Use; with G. R. Smith, M. McDonnell, S. Chen, M. D. Vera, B. E. Blass, J. C. Pelletier, V. N. Velvadapu, and J. E. Wrobel (Nov 24, 2020).

US 10,905,681. Riluzole Prodrugs and Their Use; with E. Wrobel, J. C. Pelletier, G. R. Smith, and H. Bian (Feb. 2, 2021).

US 10,981,867. EBNA1 Inhibitors and Methods Using Same; with T. E. Messick, G. R. Smith, P. M. Lieberman, M. E. McDonnell, Y. Zhang, M. Carlsen and S. Chen (Apr. 20, 2021).

US 11,052,070. Riluzole Prodrugs and Their Use; with E. Wrobel, J. C. Pelletier, G. R. Smith and Bian (July 6, 2021).

US 11,197,864. Pro-Drugs of Riluzole and Their Method of Use for the Treatment of Amyotrophic Lateral Sclerosis; with G. R. Smith (Dec. 14, 2021).

US 11,358,935. Prodrugs of Lanicemine and Their Method of Use; with J. C. Pelletier (June 14, 2022).

US 11,472,776. Quinazolines that Inhibit the Formation of Tau Oligomers and their Method of Use; with E. J. Davidowitz, J. G. Moe, H. Bian, C. Glucowski, J. Hendrix, A. S. Yehaskel, M. E. McDonnell, and H. Marie Loughran (Oct. 18, 2022).

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Marianne Carlsen, Senior Scientist